Macrogol glycerides, i.e. saturated polyglycolized glycerides are “Gelucire® type” excipients. Gelucires® are semi-solid excipients which are prepared by the alcoholysis of natural oils with polyoxyethylene glycols. Gelucires® are a mixture of mono-, di- and triglycerides (fatty acid esters of glycerol) and mono- and di-fatty acid esters of polyethylene glycol (PEG or macrogol). Fatty acid esters of glycerol and PEG esters present in Gelucires® are from long chains fatty acids (C12 to C18).
The large family of Gelucires® is characterized by a wide range of melting points of from about 33° C. to about 64° C. and by a hydrophilic lipophilic balance (HLB) of from about 1 to about 14.
The nature and proportion of each component are specific to a specific grade of Gelucires®. The grade of Gelucires® is designated by two numbers separated by a slash, the first number indicating its melting point and the second, the HLB.
Gelucires® have been used as excipients in different formulations such as in formulations of Theophilline (U.S. Pat. No. 4,988,679), Captopril (U.S. Pat. No. 5,433,951) or an HIV protease inhibitor (Aungst et al., 1994, Bull. Tech. Gattefossé, 87, 49-54).
Commercially available Gelucires® comprise Gelucire® 44/14, Gelucire® 50/13, Gelucire® 53/10, Gelucire® 50/02, Gelucire® 54/02 (also available as Precirol®), Gelucire® 62/05, Gelucire® 64/02 (also available as Precirol® WL 2155).
Benzothiazole derivatives have been found to be useful in the treatment of various disorders, e.g. disorders of the autoimmune and neuronal systems as well as inflammatory disorders (WO 01/47920, WO 03/091249 and WO 03/047570). The oral administration route is preferred, especially for chronic indications.